Title: Isonicotinic acid hydrazide derivatives: synthesis, antimicrobial activity, and QSAR studies
Authors: Judge, Vikramjeet ×
Narasimhan, Balasubramanian
Ahuja, Munish
Sriram, Dharmarajan
Yogeeswari, Perumal
De Clercq, Erik
Pannecouque, Christophe
Balzarini, Jan #
Issue Date: Jul-2012
Publisher: Birkhäuser Boston
Series Title: Medicinal Chemistry Research vol:21 issue:7 pages:1451-1470
Abstract: A series of isonicotinic acid hydrazide derivatives (1-19) was synthesized and tested in vitro for antimycobacterial activity against Mycobacterium tuberculosis and antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans, and Aspergillus niger and the results indicated that the compounds with OH, SCH3, and OCH3 groups were found to be active against the tested strains. None of the test compounds were active against a broad variety of RNA and DNA viruses at subtoxic concentrations, except 8, that showed some selective anti-reovirus-1 activity. The multi-target QSAR models were found to be effective in predicting the antimicrobial activity of the isoniazid derivatives and indicated the importance of nuclear repulsion energy (Nu.E) in explaining the antimicrobial activity of isoniazid derivatives. The developed QSAR models were validated using the external test set of synthesized derivatives.
ISSN: 1054-2523
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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